Matera M G, Rogliani P, Calzetta L, Canonica G W, Cazzola M
Unit of Pharmacology, Department of Experimental Medicine, University of Campania Luigi Vanvitelli, Naples, Italy.
Unit of Respiratory Medicine, Department of Experimental Medicine and Surgery, University of Rome Tor Vergata, Rome, Italy.
Drugs Today (Barc). 2017 Dec;53(12):633-645. doi: 10.1358/dot.2017.53.12.2736670.
Benralizumab is a humanized monoclonal antibody directed at the a subunit of the interleukin-5 receptor (IL-5R) that is under clinical development. The binding of benralizumab with the alpha chain of IL-5R results in inhibition of hetero-oligomerization of alpha and beta subunits and thus no signal transduction occurs. Consequently, this inhibition prevents proliferation of eosinophils and basophils and the cascade of events following it. Several pivotal trials have documented that benralizumab reduces asthma exacerbation rates with a significant increase in time to the next exacerbation, statistically improves prebronchodilator forced expiratory volume in 1 second (FEV1) and disease-specific health-related quality of life, and is well tolerated in patients with severe asthma and blood eosinophil counts greater than or equal to 150 cells/mcL.
贝那利珠单抗是一种针对白细胞介素-5受体（IL-5R）α亚基的人源化单克隆抗体，目前正处于临床开发阶段。贝那利珠单抗与IL-5Rα链结合会抑制α亚基和β亚基的异源寡聚化，从而不会发生信号转导。因此，这种抑制作用可防止嗜酸性粒细胞和嗜碱性粒细胞的增殖及其后续的一系列事件。多项关键试验证明，贝那利珠单抗可降低哮喘加重率，显著延长至下次加重的时间，在统计学上改善支气管扩张剂使用前1秒用力呼气量（FEV1）和疾病特异性健康相关生活质量，并且在重度哮喘且血液嗜酸性粒细胞计数大于或等于150个细胞/微升的患者中耐受性良好。
